Phosphonate and Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthases: A Structure-Guided Perspective [PDF]
Phosphonates and bisphosphonates have proven their pharmacological utility as inhibitors of enzymes that metabolize phosphate and pyrophosphate substrates. The blockbuster class of drugs nitrogen-containing bisphosphonates represent one of the best-known examples. Widely used to treat bone-resorption disorders, these drugs work by inhibiting the enzyme
Jaeok Park +3 more
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The yeast Xanthophyllomyces dendrorhous synthesizes the carotenoid astaxanthin, which has applications in biotechnology because of its antioxidant and pigmentation properties. However, wild-type strains produce too low amounts of carotenoids to be industrially competitive. Considering this background, it is indispensable to understand how the synthesis
Alcaíno Gorman, Jennifer +6 more
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The Property of a Key Amino Acid Determines the Function of Farnesyl Pyrophosphate Synthase in Sporobolomyces pararoseus NGR. [PDF]
Farnesyl pyrophosphate synthase (FPPS) catalyzes the synthesis of C15 farnesyl diphosphate (FPP) from C5 dimethylallyl diphosphate (DMAPP) and two or three C5 isopentenyl diphosphates (IPPs). FPP is an important precursor for the synthesis of isoprenoids
Wang Y +8 more
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Activation of autophagy during farnesyl pyrophosphate synthase inhibition is mediated through PI3K/AKT/mTOR signaling. [PDF]
Objectives Autophagy is divided into three phases: autophagosome engulfment of intracellular organelles and proteins, autophagosome fusion with lysosomes, and autolysosome degradation.
Han J, Huang C, Jiang J, Jiang D.
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Background & Aim: Osteoporosis is an increasing medical threat which is referred to as a systemic skeletal disorder that is characterized mainly by low bone mass and microarchitectural wear of bone tissue and strength, which eventually results in an ...
Samuel O. Olubode +8 more
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Structural characterization of substrate and inhibitor binding to farnesyl pyrophosphate synthase fromPseudomonas aeruginosa [PDF]
Robert Schnell
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Systematic characterization and functional analysis of <i>trans</i>-prenyltransferases in <i>Curcuma wenyujin</i>. [PDF]
IntroductionCurcuma wenyujin (Zingiberaceae), a medicinally significant species within the Curcuma genus, is highly regarded in traditional Chinese medicine for its rich terpenoid constituents.
Wang Q +12 more
europepmc +2 more sources
Nitrogen-containing bisphosphonate induces enhancement of OPG expression and inhibition of RANKL expression via inhibition of farnesyl pyrophosphate synthase to inhibit the osteogenic differentiation and calcification in vascular smooth muscle cells. [PDF]
Background Nitrogen-containing bisphosphonate(N-BP)had been found to inhibit the osteogenic differentiation and calcification in vascular smooth muscle cells (VSMCs), but the mechanism is not clear.
Xu W, Gong L, Tang W, Lu G.
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Crystallographic and thermodynamic characterization of phenylaminopyridine bisphosphonates binding to human farnesyl pyrophosphate synthase. [PDF]
Human farnesyl pyrophosphate synthase (hFPPS) catalyzes the production of the 15-carbon isoprenoid farnesyl pyrophosphate. The enzyme is a key regulator of the mevalonate pathway and a well-established drug target.
Park J +5 more
europepmc +2 more sources
Computational Insights into Binding of Bisphosphates to Farnesyl Pyrophosphate Synthase [PDF]
Bisphosphonates (BPs) are the most widely used and effective treatment for osteoporosis and Paget's disease. Non-nitrogen containing BPs (non-N-BPs), namely etidronate, clodronate, tiludronate, as well as nitrogen containing BPs (N-BPs), namely pamidronate, alendronate, ibandronate, risedronate, zoledronate and minodronate have been launched on the ...
Ohno, K, Mori, K, Orita, M, Takeuchi, M
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